Assay Detail
Binding
CHEMBL1063062
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from sigma1 receptor in rat liver membrane by liquid scintillation counting
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis, biological evaluation, and three-dimensional in silico pharmacophore model for sigma(1) receptor ligands based on a series of substituted benzo[d]oxazol-2(3H)-one derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 7.00 | 10.01 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473783 | — | — | 1 | 10.01 |
| CHEMBL15023 | TRIFLUPERIDOL | 2.0 | 1 | 9.10 |
| CHEMBL305187 | IFENPRODIL | 2.0 | 1 | 8.70 |
| CHEMBL559292 | — | — | 1 | 8.59 |
| CHEMBL474565 | — | — | 1 | 8.51 |
| CHEMBL472979 | — | — | 1 | 8.45 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.24 |
| CHEMBL551856 | — | — | 1 | 8.15 |
| CHEMBL559979 | — | — | 1 | 7.89 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 7.82 |
| CHEMBL559582 | — | — | 1 | 7.68 |
| CHEMBL557297 | — | — | 1 | 7.65 |
| CHEMBL474175 | — | — | 1 | 7.53 |
| CHEMBL514488 | — | — | 1 | 7.52 |
| CHEMBL559782 | — | — | 1 | 7.35 |
| CHEMBL554484 | — | — | 1 | 7.32 |
| CHEMBL472984 | — | — | 1 | 7.21 |
| CHEMBL562510 | — | — | 1 | 7.16 |
| CHEMBL549769 | — | — | 1 | 7.08 |
| CHEMBL550783 | — | — | 1 | 7.01 |
| CHEMBL564299 | — | — | 1 | 6.99 |
| CHEMBL551310 | — | — | 1 | 6.98 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 6.75 |
| CHEMBL564522 | — | — | 1 | 6.65 |
| CHEMBL563001 | — | — | 1 | 6.62 |
| CHEMBL473975 | — | — | 1 | 6.59 |
| CHEMBL570536 | — | — | 1 | 6.53 |
| CHEMBL552170 | — | — | 1 | 6.52 |
| CHEMBL474567 | — | — | 1 | 6.41 |
| CHEMBL559857 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473783 | — | Ki | = | 0.098 | nM | 10.01 |
| CHEMBL15023 | TRIFLUPERIDOL | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL305187 | IFENPRODIL | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL559292 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL474565 | — | Ki | = | 3.07 | nM | 8.51 |
| CHEMBL472979 | — | Ki | = | 3.58 | nM | 8.45 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL551856 | — | Ki | = | 7.1 | nM | 8.15 |
| CHEMBL559979 | — | Ki | = | 12.9 | nM | 7.89 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL559582 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL557297 | — | Ki | = | 22.5 | nM | 7.65 |
| CHEMBL474175 | — | Ki | = | 29.8 | nM | 7.53 |
| CHEMBL514488 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL559782 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL554484 | — | Ki | = | 48.1 | nM | 7.32 |
| CHEMBL472984 | — | Ki | = | 60.9 | nM | 7.21 |
| CHEMBL562510 | — | Ki | = | 69.4 | nM | 7.16 |
| CHEMBL549769 | — | Ki | = | 83.0 | nM | 7.08 |
| CHEMBL550783 | — | Ki | = | 97.0 | nM | 7.01 |
| CHEMBL564299 | — | Ki | = | 102.0 | nM | 6.99 |
| CHEMBL551310 | — | Ki | = | 105.0 | nM | 6.98 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL564522 | — | Ki | = | 223.0 | nM | 6.65 |
| CHEMBL563001 | — | Ki | = | 239.0 | nM | 6.62 |
| CHEMBL473975 | — | Ki | = | 258.0 | nM | 6.59 |
| CHEMBL570536 | — | Ki | = | 297.0 | nM | 6.53 |
| CHEMBL552170 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL474567 | — | Ki | = | 394.0 | nM | 6.41 |
| CHEMBL559857 | — | Ki | = | 594.0 | nM | 6.23 |
| CHEMBL551855 | — | Ki | = | 843.0 | nM | 6.07 |
| CHEMBL540232 | — | Ki | = | 871.0 | nM | 6.06 |
| CHEMBL564784 | — | Ki | = | 901.0 | nM | 6.04 |
| CHEMBL474182 | — | Ki | = | 1017.0 | nM | 5.99 |
| CHEMBL562450 | — | Ki | = | 1147.0 | nM | 5.94 |
| CHEMBL564465 | — | Ki | = | 1835.0 | nM | 5.74 |
| CHEMBL570315 | — | Ki | = | 1833.0 | nM | 5.74 |
| CHEMBL540733 | — | Ki | = | 1947.0 | nM | 5.71 |
| CHEMBL550990 | — | Ki | = | 2492.0 | nM | 5.60 |
| CHEMBL557708 | — | Ki | = | 3233.0 | nM | 5.49 |
| CHEMBL474566 | — | Ki | = | 6210.0 | nM | 5.21 |
| CHEMBL565070 | — | Ki | = | 8550.0 | nM | 5.07 |